Doxorubicin (adriamycin) is perhaps the most useful new anticancer drug in use at this time. It (along with daunorubicin) is a principal agent in the treatment of an unusually wide number of solid tumors and leukemias. Regrettably, many patients with these tumors fail to respond, and essentially no patients with some serious tumor types (colon cancer, melanoma) respond. In addition, chronic treatment produces irreversible heart damage that can be fatal if continued. Thus, there is great need for analogs which give a better rate of response, a wider spectrum of response, or reduced cardiotoxicity. More effective and less toxic agents are widely sought. The most active new analogs so far, judging from screening results in a widely used test against mouse leukemia P388 in a 3-dose treatment schedule (q4d 5,9,13), are two lipophilic derivatives (AD32 and N,N-dibenzldaunorubicin) that required significantly higher doses, and which fail to interact with DNA in vitro although DNA is believed to be a primary biological target for the anthracycline series. Reductive alkylation of doxorubicin and daunorubicin, using an aldehyde or ketone plus NaBH.sub.3 CH, has proven to be a useful chemical method for modifying the structures to give semisynthetic analogs. Most N-alkyl derivatives have been active in the antitumor screen against mouse leukemia P388, but are not significantly different from doxorubicin or daunorubicin. A few such derivatives have been inactive.